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Solid dispersion body of berberine-phospholipid complex and preparation method thereof

A solid dispersion, berberine phospholipid technology, applied in the solid dispersion of berberine phospholipid complex and its preparation, the field of berberine phospholipid complex solid dispersion, can solve the problem of small industrialization prospects and poor fluidity of solid dispersion and other issues, to achieve the effect of improving bioavailability, promoting drug absorption, and increasing fat solubility

Inactive Publication Date: 2012-11-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are reports on preparing other phospholipid complex solid dispersions as carrier materials with PVP or PEG, the solid dispersions made have poor fluidity and little industrialization prospect
And the technology of preparing phospholipid complex solid dispersion with TPGS, which not only has the effect of inhibiting the efflux of P-glycoprotein, but also has the function of carrier dispersion, combined with silicon dioxide with extremely good dispersion function as the solid dispersion carrier material, has not been reported yet.

Method used

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  • Solid dispersion body of berberine-phospholipid complex and preparation method thereof
  • Solid dispersion body of berberine-phospholipid complex and preparation method thereof
  • Solid dispersion body of berberine-phospholipid complex and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Prescription: Berberine 50mg, Phospholipids 100mg, TPGS 50mg, Silicon Dioxide 6mg

[0032] Preparation process: take 50 mg of berberine and 100 mg of phospholipids, dissolve them in 100 ml of ethanol, and react under magnetic stirring at 40°C for 2 hours, then add 50 mg of TPGS, dissolve them in ethanol, stir and dissolve evenly, then add 6 mg of silicon dioxide, Stir for 30 minutes to make full contact and mix uniformly. Using the solvent-reduced-pressure drying method, the mixed solution after the reaction was placed on a rotary evaporator, and the reaction solvent was evaporated under reduced pressure at 40° C., and the residue was continued to be dried under reduced pressure at room temperature overnight. Finally, a solid dispersion of berberine phospholipid complex with a mass ratio of 1:2:1 was obtained, which contained 3% silicon dioxide.

Embodiment 2

[0034] Prescription: Berberine 50mg, Phospholipids 150mg, TPGS 100mg, Silicon Dioxide 15mg

[0035] Preparation process: Take 50mg of berberine and 150mg of phospholipids, dissolve them in 100ml of ethanol, and react under magnetic stirring at 40°C for 2 hours, then add 100mg of TPGS, dissolve them in ethanol, stir and dissolve evenly, then add 15mg of silicon dioxide, Stir for 30 minutes to make full contact and mix uniformly. The solvent-reduced pressure drying method was also used to remove the reaction solvent ethanol. Finally, a solid dispersion of berberine phospholipid complex with a mass ratio of 1:3:2 was obtained, which contained 5% silicon dioxide.

Embodiment 3

[0037] Prescription: Berberine 50mg, Phospholipids 200mg, TPGS 250mg, Silicon Dioxide 25.0mg

[0038] Preparation process: take 50mg of berberine, 200mg of phospholipids, dissolve in 100ml of ethanol, reflux with magnetic stirring at 40°C for 2 hours, add 250mg of TPGS, dissolve in ethanol, stir and dissolve evenly, then add 25.0mg of silicon dioxide , Stir for 30 minutes to make full contact and mix uniformly. Using the solvent-freeze-drying method, the reacted mixture was pre-frozen in a refrigerator at -20°C for 12 hours, quickly transferred into a freeze dryer, and freeze-dried under vacuum for 48 hours. Finally, a solid dispersion of berberine phospholipid complex with a mass ratio of 1:4:5 was obtained, which contained 5% silicon dioxide.

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Abstract

The invention discloses a solid dispersion body of a berberine-phospholipid complex and a preparation method thereof and belongs to the field of pharmaceuticals. The lipid solubility of berberine is low, the absorbing capability of a permeable membrane is poor, and the berberine is a substrate of P-glycoprotein (P-gp) and is expelled by epithelial cells on the stomach and intestine to result in the extremely low oral bioavailability, so that an effective method needs to be adopted to improve the lipid solubility of the berberine, meanwhile, the expelling of P-glycoprotein is inhibited, and further the drug absorption is promoted. The solid dispersion body of the berberine-phospholipid complex disclosed by the invention consists of berberine, phospholipid, vitamin E polyethylene glycol succinic acid ester and silicon dioxide in a certain weight ratio, and has the advantages that the lipid solubility of the berberine is improved, the expelling of P-glycoprotein is inhibited, the drug is promoted to be absorbed by the gastrointestinal tract, the bioavailability is improved, the stability and the flowability are good, the preparation method is simple and convenient, and the great industry prospect is provided.

Description

technical field [0001] The invention relates to a berberine phospholipid complex solid dispersion and a preparation method thereof, in particular to a berberine phospholipid complex solid dispersion with TPGS and silicon dioxide as a mixed carrier, belonging to the pharmaceutical field. Background technique [0002] Berberine (Berberine) is a main component of Chinese medicine Coptis chinensis, and it also mainly exists in other plants such as Phellodendron Phellodendri and Three Needles. Berberine is a quaternary ammonium alkaloid with the molecular formula C 20 h 18 NO 4 , the chemical structure is as follows: [0003] [0004] The pharmacological activity of berberine is very rich, and the antibacterial and anti-inflammatory effects of berberine are the most clinically used. In recent years, there have been continuous literature reports that berberine can also achieve anti-arrhythmia, anti-tumor, and anti-inflammatory effects after being absorbed into the blood. Hi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4375A61K47/34A61K47/04A61P29/00A61P31/04
Inventor 吕慧侠陈燕张振海周建平
Owner CHINA PHARM UNIV
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